About 34 results found for searched term "K-Ras-IN-1" (0.221 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M20595 | K-Ras(G12C) inhibitor 12 | ROCK |
| K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C). | ||
| M20708 | K-Ras-IN-1 | Ras |
| MDK-3017 | ||
| K-Ras-IN-1 inhibits K-Ras by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure. | ||
| M42117 | KRAS G12C inhibitor 61 | ERK |
| KRAS G12C inhibitor 61 inhibits phospho-ERK 1/2 in MIA PaCa-2 cells with an IC50 value of 9 nM. | ||
| M55018 | RMC-9805 | Ras |
| KRAS G12D inhibitor 18 | ||
| RMC-9805 (KRAS G12D inhibitor 18) is an orally active KRAS G12D inhibitor. RMC-9805 (KRAS G12D inhibitor 18) inhibits RAS signaling and induces apoptosis in KRAS G12D mutant cancer cells. | ||
| M1664 | AZD2281 (Olaparib) | PARP |
| Olaparib; KU-0059436 | ||
| AZD 2281 (Olaparib, KU-0059436) is a potent PARP (poly ADP-ribose polymerase) inhibitorwith IC50 of 5 and 1 nM for PARP-1and PARP-2 respectively. Olaparib is an autophagy and mitophagy activator. | ||
| M2199 | Camptothecin | Topoisomerase |
| Camptothecine; (S)-(+)-Camptothecin; CPT | ||
| Camptothecin (CPT), an alkaloid, is an inhibitor of DNA Topoisomerase I (Topo I) with an IC50 value of 679 nM. Camptothecin (CPT) has strong antitumor activity against colorectal cancer, breast cancer, lung cancer and ovarian cancer, and modulates hypoxia-inducible factor-1α (HIF-1α) activity by altering miRNA expression patterns in human cancer cells. | ||
| M2595 | Raltegravir | Integrase |
| MK-0518 | ||
| Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM, respectively. | ||
| M2557 | Ezatiostat | Apoptosis |
| TER199, TLK199 | ||
| Ezatiostat (TER199, TLK199) is a glutathione analog inhibitor of glutathione S-transferase (GST) P1-1. Ezatiostat leads to JNK activation by inhibiting GSTP1. Ezatiostat stimulates both lymphocyte production and bone marrow progenitor proliferation. | ||
| M2587 | JW55 | PARP |
| JW 55 is an inhibitor of the PARP domain of tankyrase 1 and 2 (TNKS1/2). JW55 decreased auto-PARsylation of TNKS1/2 in vitro with IC50 values of 1.9 uM and 830 nM respectively. | ||
| M2608 | Kobe0065 | Ras |
| Kobe0065 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD, exhibits potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM. | ||
| M3195 | MK-2048 | Integrase |
| MK-2048 is a potent inhibitor of integrase (IN) and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively. | ||
| M3484 | Dolutegravir | Integrase |
| GSK1349572 | ||
| Dolutegravir (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H. | ||
| M3663 | K-Ras(G12C) inhibitor 9 | Ras |
| K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C). | ||
| M4030 | Crassicauline-A | Others |
| Crassicaulin A | ||
| Crassicauline A (Crassicaulin A) is A bioactive alkaloid in aconite roots. Crassicauline A (Crassicaulin A) had antifeedant activity against the adult Raptor, and its EC50 value was 1134.5 PPM. | ||
| M4532 | Rhodionin | AChR/AChE |
| Rhodionin was isolated from the roots of Rhodiola crenulata and is a specific non-competitive cytochrome P450 2D6 inhibitor with IC50 of 0.761 μM and Ki of 0.769 μM. Rhodionin effectively inhibited acetylcholinesterase (AChE) in a dose-dependent manner with an IC50 range of 57.50 to 2.43 μg/mL. Rhodionin had effective DPPH radical scavenging activity with IC50 of 19.49 μM. | ||
| M4556 | Fraxinellone | PD-1/PD-L1 |
| Fraxinellone was isolated from the root bark of the brassica family Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor that inhibits HIF-1α synthesis without affecting HIF-1α degradation. Fraxinellone has potential for cancer immunity by targeting PD-L1. | ||
| M10593 | MRTX1133 | Ras |
| MRTX-1133 | ||
| MRTX1133 is a first-in-class, potent and highly selective KRAS G12D inhibitor. MRTX1133 targets the KRAS G12D protein in both active and inactive states. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. | ||
| M5267 | E7449 | PARP |
| Stenoparib; 2X-121; MGI25036 | ||
| E7449 is an orally bioavailable, brain penetrable, small molecule dual inhibitor of PARP1/2 that also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1/2), important regulators of canonical Wnt/β-catenin signaling. It has IC50 values of 1.0 and 1.2 nM for PARP1 and 2, respectively. | ||
| M5852 | Lifitegrast | Integrin |
| SAR 1118; Xiidra | ||
| Lifitegrast is an antagonist of integrin lymphocyte function associated antigen-1 (LFA-1). The IC50 of Jurkat T cells to icAM-1 was 2.98nM. Lifitegrast blocks the interaction between LFA-1 and ICAM-1, thereby reducing T cell activity and cytokine secretion. | ||
| M8601 | R-Ketorolac | Others |
| R-Ketorolac is potent and selective Rho-family GTPases Cdc42 (cell division control protein 42) and Rac1 (Ras-related C3 botulinum toxin substrate 1) allosteric inhibitor that modulates downstream GTPase-dependent physiologic responses critical to tumor metastasis. | ||
| M11233 | Recombinant Human KRAS(G12C, His, E.coli) | Recombinant Proteins |
| Ki-Ras; c-K-ras; KRAS2 | ||
| Recombinant Human KRAS(G12C, His, E.coli) was produced by the Escherichia coli expression system, and the target gene encoding Thr2-CYS185 (Gly12Cys) was expressed by 6His tag at the N-terminal. | ||
| M8654 | AA-CW236 | Others |
| AA-CW236 is a cell-permeable chloromethyl triazole (CMT) derivative that acts as a non-pseudosubstrate inhibitor against human O(6)-alkylguanine DNA methyltransferase (MGMT) by targeting MGMT active site Cys145 for covalent modification (KI = 24 nM, kinact = 0. | ||
| M9359 | BAY-293 | Ras |
| BAY293 | ||
| BAY-293 is a potent inhibitor of Son of Sevenless 1 (SOS1), blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC50 of 21 nM. | ||
| M9768 | MK-7622 | AChR/AChE |
| MK-7622 is a cholinesterase inhibitor, it is also a muscarinic M1 receptor positive allosteric modulator. | ||
| M9801 | BI-3406 | Ras |
| BI-3406 is a highly potent and selective SOS1::KRAS inhibitor (IC50=6 nM), which selectively binds to SOS1 and blocks the interaction with KRAS, irrespective of the KRAS mutation. | ||
| M9910 | CDKI-73 | CDK |
| CDKI73; Asnuciclib; LS-007 | ||
| Cdki-73 (LS-007) is an orally active and highly effective CDK9 inhibitor with Ki values of 4 nM, 4 nM and 3 nM against CDK9, CDK1 and CDK2, respectively. Cdki-73 down-regulates phosphorylation of RNA polymerase II. Cdki-73 is also an inhibitor of Rab11. | ||
| M10561 | IMP-1088 | DNA/RNA Synthesis |
| IMP1088 | ||
| IMP-1088 is a novel potent and selective blocker of N-myristoylation in cells. IMP-1088 is also a potent human N-myristoyltransferases NMT1 and NMT2 dual inhibitor with IC50s of <1 nM for HsNMT1 and HsNMT2. | ||
| M10600 | SAH-SOS1A TFA | Ras |
| SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM) and directly and independently blocks nucleotide association. | ||
| M10637 | GSK3368715 2HCl | PRMTs |
| EPZ019997 2HCl | ||
| GSK3368715 2HCl is a novel potent, orally active, reversible type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50 values of 3.1 nM, 48 nM, 1148 nM, 5.7 nM and 1.7 nM for PRMT1, PRMT3, PRMT4, PRMT6, PRMT8, respectively. | ||
| M10882 | RMC-0331 | Others |
| RM-023 | ||
| RMC-0331 (RM-023) is a highly potent, selective, and oral bioavailable SOS1 inhibitor. RMC-0331 is an in vivo tool compound that blocks RAS activation by disrupting RAS-SOS1 interactions. | ||
| M11109 | 3-O-Methylquercetin | PDE |
| 3',4',5,7-tetrahydroxy-3-methoxyflavone | ||
| 3-O-Methylquercetin (3-MQ), a main constituent of Rhamnus nakaharai, inhibits total cAMP and cGMP-phosphodiesterase (PDE) of guinea pig trachealis. 3-O-Methylquercetin (3-MQ) exhibits IC50 values of 31.9 μM， 86.9 μM， 18.6 μM and 1.6 μM for PDE1, PDE5, PDE2 and PDE4, respectively. | ||
| M11185 | 3-Deazaadenosine hydrochloride | Others |
| 3-DZA HCl, c3Ado HCl | ||
| 3-deazaadenosine HCl (3-DZA, c3Ado) is an effective s-adenosylhomocysteine hydrolase inhibitor with Ki value of 3.9 μM. 3-deazaadenosine HCl inhibits the transcription of TNF-α and IL-1β induced by bacterial liposolysaccharide. 3-deazaadenosine HCl inhibits NF-κB transcriptional activity, prevents CARBOxyl methylation of Ras induced by FCS, and reduces ERK1/2 and Akt phosphorylation induced by FCS. | ||
| M11427 | RM-018 | Ras |
| INDEX NAME NOT YET ASSIGNED | ||
| RM-018 is an inhibitor of the active state of KRASG12C. Rm-018 retains the ability to bind and inhibit KRASG12C/Y96D. Rm-018 combines with GTP-bound to activate the [" RAS(ON) "] state of KRASG12C. | ||
| M11442 | Divarasib | Ras |
| GDC-6036 | ||
| Divarasib (GDC-6036) is an orally active, selective, covalently mutated KRAS G12C inhibitor with an IC50<0.01 μM for K-Ras G12C. GDC-6036 has an EC50 of 2 nM in K-Ras G12C-alkylated HCC1171 cells. can be used in studies related to non-small cell lung cancer ( NSCLC) related studies. | ||
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